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顺式二氯二氨铂(顺铂,Cisplatin)于本世纪60年代被发现有抑瘤作用,其高度的活性及广谱性使之成为人类抗癌剂中应用最为广泛的一种。然而,它的肾毒性、神经毒性、耳毒性较大。并且,许多原先对它敏感的肿瘤会在治疗过程中产生耐药性。这就使得全球范围内都在致力寻找具有更高治疗指数和对耐顺铂的肿瘤有效的铂类似物,并且取得了一定的进展。其中,脂质体包裹的顺二新癸酸反右旋环己二胺铂(L-NDDP)的合成和应用就是一例。与顺铂相比,L-NDDP毒性小、疗效好,与顺铂没有交叉耐药性。目前,国外对它已经完成了一期临床试验,而国内还未见有关报道。本文在此对其药理学研究作一回顾。
Cisplatin (cisplatin, Cisplatin) in the 60s of this century was found to have anti-tumor effect, its high activity and broad spectrum make it the most widely used in human anticancer drugs. However, its nephrotoxicity, neurotoxicity and ototoxicity are greater. And, many of the tumors that were previously sensitive to it developed resistance during the course of treatment. This makes global efforts to find platinum analogs with higher therapeutic index and effective on cisplatin-resistant tumors, and some progress has been made. Among them, the synthesis and application of liposomal cis-neodecano-cyclohexene diamine (L-NDDP) is an example. Compared with cisplatin, L-NDDP small toxicity, good effect, and cisplatin no cross-resistance. At present, it has completed a phase of clinical trials abroad, but the country has not seen the relevant reports. Here’s a review of its pharmacology.